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Synthesis of Asp-based lactam cyclic peptides using an amide-bonded diaminodiacid to prevent aspartimide formation

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00472H, Communication
Wen-Jie Li, Jun-You Chen, Hui-Xia Zhu, Yi-Ming Li, Yang Xu
A diaminodiacid (DADA) containing an amide bond can be used in Fmoc solid-phase peptide synthesis (SPPS) of an Asp-based lactam cyclic peptide with no aspartimide formation.
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Synthesis of alkenylphosphine oxides via Tf2O promoted addition–elimination of ketones and secondary phosphine oxides

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00318G, Communication
Jiangkai Ma, Lianjie Wang, Anjiang Qiao, Zhongxian Li, Fengqian Zhao, Junliang Wu
An efficient method for the synthesis of alkenylphosphine oxides via the addition-elimination of SPOs to ketones has been developed. The reaction exhibits good yields and compatibility. Several conversions have also proven the value of this method.
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Electrochemical nickel-catalyzed cross-coupling of glycosyl thiols with preactivated phenols and ketones

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00442F, Communication
Fuxin Li, Hui Liu, Wanyu Xing, Qingju Zhang, Liming Wang
Here we report an efficient electrochemical nickel-catalyzed cross-coupling reaction for the synthesis of S-glycosides from preactivated phenols and ketones.
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Stereoselective Synthesis of gem-Dihalopiperidines via Halo-Aza-Prins Cyclization Reaction: Access to Piperidin-4-ones and Pyridines

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00338A, Paper
Anil Kumar Saikia, Surjya Kumar Bora, Subhamoy Biswas, Bipin Kumar Behera
An efficient methodology for the synthesis of 4,4-dihalopiperidine derivatives has been developed from N-(3-halobut-3-en-1-yl)-4-methylbenzenesulfonamide and aldehyde catalyzed by In(OTf)3 in excellent yields. The reaction involves an initial formation of six...
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Hydrosilylation of nitriles and tertiary amides using a zinc precursor

Org. Biomol. Chem., 2024, 22,3053-3058
DOI: 10.1039/D4OB00161C, Paper
Ravi Kumar, Rohan Kumar Meher, Himadri Karmakar, Tarun K. Panda
A competent and selective hydrosilylation of nitriles and tertiary amides catalyzed by zinc bis(hexamethyldisilazide) [Zn(HMDS)2] under solvent-free and mild conditions are reported, as a sustainable and desirable alternative to existing methods.
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Unusual immunosuppressive pyridine-containing bisnor- (c23), tetranor- (c21) and pentanor- (c20) sesterterpenoids from Tibetan Leucosceptrum canum

Org. Biomol. Chem., 2024, 22,3019-3024
DOI: 10.1039/D4OB00334A, Paper
Man Li, Ling Feng, Han Zhang, Yan-Chun Liu, Ting-Ting Zhou, Yu Zheng, Kai Guo, Yan Liu, Sheng-Hong Li
Six unusual pyridine-containing bisnor- (C23), tetranor- (C21) and pentanor- (C20) sesterterpenoids were obtained from the medicinal plant Leucosceptrum canum of Tibetan origin. The immunosuppressive activities of these sesterterpenoids were observed.
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Synthesis of alkynyl sulfides via base-promoted nucleophilic ring-opening of α-bromostyrene sulfonium salt

Org. Biomol. Chem., 2024, 22,2953-2957
DOI: 10.1039/D4OB00203B, Communication
Junqi Zhou, Ziyu Wang, Hanmiao Xu, Mengke Su, Jian Wen
An effective method for synthesizing various alkynyl sulfides has been developed using tetramethylene sulfoxide as a sulfur source through base-promoted nucleophilic ring-opening reactions.
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Selective enhancement of (6–4) photoproduct formation in dithymine dinucleotides driven by specific sugar puckering

Org. Biomol. Chem., 2024, 22,3025-3034
DOI: 10.1039/D4OB00279B, Paper
Jouda Jakhlal, Clément Denhez, Stéphanie Coantic-Castex, Agathe Martinez, Dominique Harakat, Thierry Douki, Dominique Guillaume, Pascale Clivio
Evidence is presented that (6–4) photoproduct formation between two thymine residues in dinucleotide analogues is significantly and specifically enhanced when the 5''- and 3''-end sugar puckering are mainly north and south, respectively.
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Photochromism of phenazine-2,3-diol derivatives through excited state intermolecular proton transfer based on keto–enol tautomerization

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00387J, Paper
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Kazuki Ohira, Kumpei Kozuka, Naoki Kaneda, Masahiro Yamamoto, Keiichi Imato, Yousuke Ooyama
It was found that phenazine-2,3-diol derivatives exhibit photochromism through excited state intermolecular proton transfer (ESInterPT) processes based on keto–enol tautomerization.
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Charge-transfer inclusion complex formation of the tropylium cation with prism[6]arenes

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00423J, Communication
Guojiao Zhang, Channi Cheng, Zhengxiang Li, Dezhi Zhao, Chengyou Han
We report that charge-transfer (CT) inclusion complexes were formed between prism[6]arenes and tropylium cation. Additionally, the CT complex showed Cl/Ag+ responsiveness which can be easily monitored by the naked eye.
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Nickel-catalysed regio- and stereoselective hydrocyanation of alkynoates and its mechanistic insights proposed by DFT calculations

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00380B, Communication
Shigeru Arai, Koichi Nakazawa, Xiao-Fei Yang, Masaya Nakajima, Shinji Harada, Atsushi Nishida
This work discloses the origin of regio- and stereoselectivity of hydrocyanation of alkynoates.
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Exploring the mechanism of the reductive amination of acetophenones via Borch approach: the role of the acid catalyst

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00160E, Paper
João Pedro Albuquerque Souza, Amanda Krauskopf Jacobs, Leandro Piovan, Renan Borsoi Campos
The energetic viability of several mechanistic variations of the reductive amination of acetophenones via the Borch approach was reexamined through density functional theory calculations. The crucial involvement of the acid...
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Dess–Martin periodinane-mediated oxidation of the primary alcohol of cytidine into a carboxylic acid

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00240G, Communication
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Alexandra R. E. Serre, Vibhu Jha, Adèle Rivault, Leif A. Eriksson, Goreti Ribeiro Morais, Robert A. Falconer
Herein we describe the first example of the conversion of the primary alcohol of cytidine into a carboxylic acid by use of the Dess–Martin periodinane oxidising agent.
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Photoproperties of Favipiravir and their 6-Substituted Analogues: Fluorescence Controlled through Halogen Substitution and Tautomerism

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00397G, Paper
Angel H Romero, Marcos Couto, Ivan E Romero, German Fuentes, Matías N. Möller
Herein, we showed the photophysical properties of the favipiravir and their 6-substituted analogues. Also, we interpreted the origin of the fluorescence of the favipiravir and their 6-substituted analogues as function...
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Natural products from human microbiome: an emergent frontier in organic synthesis and drug discovery

Org. Biomol. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4OB00236A, Review Article
Goverdhan Mehta, Saumitra Sengupta, Srihari Pabbaraja
Often referred to as “second genome”, human microbiome is at the epicenter of a complex inter-habitat biochemical network, such as the “gut-brain axis”, which have emerged as significant determinant of...
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TEMPO/PhI(OAc)2 promotes the α-aminophosphinoylation of alcohols with amines and H-phosphine oxides in aqueous medium

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00302K, Communication
Qiang Huang, Xin Jin, Lvjia Wu, Jiangdong Li, Qianlu Xing, Xianheng Wang, Changkuo Zhao
The aminophosphinoylation of alcohols with amines and H-phosphine oxides provides an efficient and mild approach to access various α-aminoalkylphosphine oxides in good yields with good tolerance of functional groups using H2O as a clean solvent.
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Measuring local pH at interfaces from molecular tumbling: A concept for designing EPR-active pH-sensitive labels and probes

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00167B, Paper
Open Access
Maxim A. Voinov, Nicholas Nunn, Roshan Rana, Atli Davidsson, Alex I. Smirnov, Tatyana I. Smirnova
EPR-based local pH measurements based on changes in rotational dynamics of spin-bearing molecules upon protonation.
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Sustainable preparation of 2-acylbenzothiazoles under the cooperation of ionic liquids and microwave irradiation

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00315B, Paper
Shoushun Wang, Mengjie Liu, Yiyuan Yue, Xiude Hu, Yalin Zhang, Guodong Shen, Ruiguo Dong, Lilong Shi, Bing Yu, Xianqiang Huang
A series of 2-acylbenzothiazole derivatives were sustainably synthesized for the first time under the cooperation of ionic liquids and microwave irradiation, metal- and extra-additives-free conditions.
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Base- and sulfur-promoted oxidative lactonization of chalcone-acetate Michael adducts: access to pyran-2-ones

Org. Biomol. Chem., 2024, Advance Article
DOI: 10.1039/D4OB00479E, Communication
Cao Nguyen Nguyen, Duc Toan Nguyen, Ha An Tran, Dinh Hung Mac, Thi Thu Tram Nguyen, Pascal Retailleau, Thanh Binh Nguyen
A cost-effective, practical, straightforward and scalable synthesis of α-pyrones via base- and sulfur-promoted annulation of phenylacetates and chalcones is reported.
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As the price of aviation turbine fuel soars, airlines’ finances spin out of control




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Omicron: Airlines on a wing and prayer

Over 3,000 flights were cancelled on the eve of Christmas and cancellations are expected to double as New Year approaches




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2022 holds promise for the airline sector

Omicron might dent growth, but the long-term outlook seems promising




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As India builds its newest airports, it needs robust, fail-proof SOPs

A near air mishap on Bengaluru skies that put the lives of 430 people in danger shows safety risk norms require constant refresh




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Profits offer hope of soft landing to Spicejet

Apart from swift settlement with former owners, the airline urgently needs an immediate infusion of cash




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Corporate travel is unlikely to reach pre-Covid levels

However, with offices opening up, many airlines are seeing increased demand with an uptick for premium cabins




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First-ever gravity-defying plane swap set for April 24

Two pilots will swap planes mid-air




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How cabin pressure plays a key role

Ensures adequate levels of oxygen in the air




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Air infrastructure plans should be future-proof

India’s aviation story is full of delayed, untapped and under-utilised potential




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Why has private capital not been taken to Indian aviation 

With banks becoming increasingly cautious and credit flows tightening, private capital must be explored and enticed




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Youtube introduces shopping affiliate programme for eligible Indian creators via Flipkart and Myntra

As more platforms allow creators to earn from viewers’ purchases of featured products, YouTube also announced its Shopping affiliate programme in India




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Apple AirPods Pro’s new hearing aid feature could help people face a problem they’d rather ignore

Millions who could benefit from hearing aids have never tried them, but the Apple AirPods could change this




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Jio’s Diwali Dhamaka plan offers year-long prepaid plan for ₹3,599

Jio is offering a prepaid plan of 2.5 GB of data per day for an entire year, priced at₹3,599, as part of a Diwali offer




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Google’s moneymaking machine still pumping out massive profits despite multiple threats

Google is still thriving while the company navigates through a pivotal shift to artificial intelligence and battles regulators trying to topple its internet empire




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Amazon's improving retail sales boost third-quarter profit, revenue beats estimates

Like its tech peers, Amazon said it expected higher capital expenditures for the foreseeable future to help develop artificial intelligence software




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Perplexity AI CEO says “still haven’t gotten” a green card amid immigration debate ahead of U.S. Presidential Election 2024

Srinivas went on to work with OpenAI for a year before co-founding Perplexity AI in 2022




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Centre eyes ‘presumed consent’ for cornea retrieval in hospital deaths

THOTA may be amended to facilitate retrieval of cornea from all Indians who die in hospitals, without family consent. 




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Why did the Centre sanction a 50% hike in prices of commonly-used drugs?

According to the government the recent 50% hike in prices of eight drugs was sanctioned keeping in mind the larger public interest and to ensure continued availability of drugs




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Trachoma eliminated as a public health problem in India; what next?

The achievement marks a significant public health victory and has profound economic implications. Trachoma’s impact, through blindness and visual impairment, results in an estimated economic loss of $2.9 to 5.3 billion annually due to reduced productivity




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Drugs regulator finds 49 samples not of standard quality, manufacturers asked to withdraw their products

Four spurious drugs were also found and action has been initiated against the makers, the DCGI said




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What is stereotactic radiation therapy for prostate cancer? How does it compare to other treatments?

Stereotactic radiotherapy uses high doses of radiation to target and kill cancer cells; it uses newer machines that can deliver very focused radiation beams




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Roll back approval to import used medical devices, med-tech industry urges PM

The group said the move puts at risk patient safety and undermines the domestic med-tech sector. It said that refurbished machines are not subject to stringent quality checks applicable to new devices.




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Doctors stress healthy lifestyle, regular check-up to prevent strokes in young adults

The webinar was held as part of The Hindu’s Wellness Series




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National Pharmaceutical Pricing Authority directs firms to cut prices of three anti-cancer drugs

Govt. had earlier scrapped customs duty on Trastuzumab, Osimertinib and Durvalumab and also reduced GST rates on them




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ICMR invites expression of interest from firms for making anaemia detection device

The council wants to expand the effective screening network of anaemia among different age populations across India




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Following WHO guidelines for sodium content in packaged food could prevent 3 lakh deaths in India in 10 years: study

Additionally, about 1.7 million new cardiovascular disease cases and 7,00,000 new chronic kidney disease cases could be prevented compared to current practices, the study said




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Doctors urge National Medical Commission to simplify centralised registration process

The register is a centralised repository that contains the name, address, and qualifications of licensed medical practitioners; however the registration process is complex and cumbersome, say doctors




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Stop abuse of patent monopolies in rare diseases, say patient representatives and treatment activists 

They seek urgent intervention by government, courts, and lawmakers into the issue  




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Bengaluru start-up strives to bridge India’s genomics data gap to aid precision oncology

The company, 4baseCare, has come up with a gene panel for the Indian population after extensive research. This, according to the founders, will allow doctors to provide more evidence-based and data-backed treatment for cancer patients in the country




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Osteoporosis can shorten your life − here’s how to prevent fractures and keep bones healthy

The key to having healthy bones for a lifetime is to take some simple preventive measures – and the earlier, the better




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Can mid-level healthcare providers compensate for physician shortages in rural India?

To make up for doctor shortages, several countries around the world have introduced a cadre of MLHPs into their health systems; however, in India, mainstreaming of MLHPs has time and again been met with resistance from organised medicine